Exploring Nitrostyrene as a Scaffold for a New Class a of Monoamine Oxidase Inhibitors

• Type: Article in International Scientific Journal
• Date: 2012

Authors

reis, joana (Author) Other; oliveira, catarina (Author) Other; milhazes, nuno (Author) Other; vina, dolores (Author) Other; borges, fernanda (Author) FCUP

Journal

Title: Letters in Drug Design & Discovery

Vol. 9

Pages: 958-961

ISSN: 1570-1808

Publisher: Bentham Science

Indexing

ISI Web of Knowledge - 1 Citation

Scopus - 1 Citation

Scientific classification

FOS: Natural sciences > Chemical sciences

CORDIS: Physical sciences > Chemistry > Applied chemistry > Pharmaceutical chemistry

Other information

Authenticus ID: P-002-35P

DOI: 10.2174/157018012804586888

Abstract (EN): With the ultimate purpose of finding out the structural features that are relevant for MAO inhibitory activity and selectivity towards MAO-B isoform, a series of compounds encompassing a beta-nitrostyrene moiety was designed and the in vitro inhibitory activity was evaluated. In the present work, we report the synthesis and the pharmacological evaluation of a series of functionalized derivatives of beta-methyl-beta-nitrostyrene with distinct substitution patterns in the phenyl ring, namely hydroxyl, methoxy, benzyloxy and methylenedioxy. All the studied compounds were substituted in meta and para positions of the phenyl ring related to the nitrovinyl side chain. The synthesized compounds were evaluated towards both human MAO isoforms, displaying some of them activities in the low micromolar range. Particularly compound 6 (a methylenedioxy derivative) exhibits high potency and selectivity towards MAO-B.

Language: English

Type (Professor's evaluation): Scientific